Synthetic method for adefovir dipivoxil

A technology of adefovir dipivoxil and a synthesis method, which is applied in the synthesis field of adefovir dipivoxil, can solve the problems of difficult control, low total yield, complicated operation and the like, and achieves the advantages of convenient operation, mild reaction conditions and high purity. Effect

Inactive Publication Date: 2014-05-21
姜丹宁
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Problems solved by technology

This route is more cumbersome to operate, difficult to control, and the total yield is lower

Method used

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Embodiment Construction

[0015] The synthetic method of adefovir dipivoxil of the present invention is.

[0016] 1. Synthesis of diethyl phosphite.

[0017] 2. Diethyl p-toluenesulfonyloxymethylphosphonate.

[0018] 3. Synthesis of 9-(2-hydroxyethyl)adenine.

[0019] 4. Synthesis of 9-[2-(diethylphosphonomethoxy)ethyl]adenine.

[0020] 5. Synthesis of adefovir.

[0021] 6. Synthesis of adefovir dipivoxil.

[0022] Add adefovir, chloromethyl pivalate, 88g of N-methylpyrrolidone and 31g of triethylamine to the reaction flask respectively, stir at room temperature for 12h, then heat up to 50-60°C and stir for 4h; cool to room temperature, add 250 mL of isopropyl acetate, stirred at room temperature for 1 to 2 hours; filtered, the filter cake was washed with 50 mL of isopropyl acetate, the filtrate was washed with saturated aqueous sodium chloride solution, the obtained organic layer was dried with sodium sulfate, and stood overnight; filtered, Concentrate the filtrate under reduced p...

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Abstract

The invention relates to an improved synthetic method for adefovir dipivoxil. The synthetic method for adefovir dipivoxil provided by the invention has the advantages of mild reaction conditions, convenient operation and high yield. The synthetic method comprises the following steps: step 1, synthesis of diethyl phosphite; step 2, synthesis of diethyl p-toluenesulfonyloxymethylphosphonate; step 3, synthesis of 9-(2-hydroxyethyl)adenine; step 4, synthesis of 9-[2-(diethylphosphonomethoxy)ethyl]adenine; step 5, synthesis of adefovir; and step 6, synthesis of adefovir dipivoxil.

Description

technical field [0001] The invention relates to an improvement of a synthetic method of adefovir dipivoxil. Background technique [0002] Adefovir dipivoxil, chemical name [[2-(6-amino-9H-purin-9-yl) ethoxy] methyl] phosphate bis-(pivaloyloxymethyl) ester, is GileadSciences of the United States The nucleoside virus inhibitor developed by the company was approved by the FDA for the treatment of hepatitis B in September 2002. It is the first new drug for the treatment of chronic hepatitis B approved by the FDA in recent years. Adefovir dipivoxil is an ester prodrug of adefovir, which is rapidly converted into adefovir in the body after oral administration. It has broad-spectrum antiviral activity and can effectively inhibit hepatotropic virus, retrovirus and herpes virus. It is clinically used to treat hepatitis B virus (HBV) infection, and has good curative effect on wild HBV and lamivudine (1amivudine)-resistant HBV. [0003] Regarding the synthesis of adefovir dipivoxil, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561
Inventor 姜丹宁戴媛媛
Owner 姜丹宁
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